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Variations in tissue selectivity amongst insulin secretagogues: a systematic review

Journal

DIABETES OBESITY & METABOLISM
Volume 14, Issue 2, Pages 130-138

Publisher

WILEY
DOI: 10.1111/j.1463-1326.2011.01496.x

Keywords

insulin secretagogues; ischaemic preconditioning; sulfonylurea receptor

Funding

  1. Canadian Diabetes Association [OG-2-09-2693-SS]
  2. Blanch/Wirtanen/Alberta Diabetes Foundation/Alberta Diabetes Institute
  3. Alliance for Canadian Health Outcomes Research in Diabetes (ACHORD)
  4. Heart and Stroke Foundation of Canada
  5. Canadian Institutes of Health Research

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Aim: Insulin secretagogues promote insulin release by binding to sulfonylurea receptors on pancreatic beta-cells (SUR1). However, these drugs also bind to receptor isoforms on cardiac myocytes (SUR2A) and vascular smooth muscle (SUR2B). Binding to SUR2A/SUR2B may inhibit ischaemic preconditioning, an endogenous protective mechanism enabling cardiac tissue to survive periods of ischaemia. This study was designed to identify insulin secretagogues that selectively bind to SUR1 when given at therapeutic doses.

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